Current Medicinal Chemistry - Central Nervous System Agents - Volume 4, Issue 3, 2004

Central nervous system (CNS)-related pathologies have been one of the most ongoing challenges for scientists. Traditionally, these disorders have been studied from the point of view based on the therapeutic control of the classical and oldknown neurotransmitter systems. However, neurodegenerative diseases, pain and neuroprotection are examples of disorders which still need important efforts and better solutions Read More

The inactivation of anandamide, the main and most widely studied endocannabinoid to date, has progressively gained support as a process of crucial importance in controlling the biological action both in time and place of this Nacylethanolamine. Within the components that account for the inactivation of anandamide, the membrane anandamide transporter (ANT) constitutes a focus of major attention since it represents one Read More

There is a good evidence to suggest that activation of cannabinoid receptors may be beneficial not only in the treatment of conditions such as pain, but even in neurodegenerative states, such as in stroke and trauma. Nevertheless, the major obstacle to the development of cannabinoid receptor agonists as therapeutic agents for the treatment of such disorders the psychomotor are effects resulting from cannabinoid receptor acti Read More

New data strengthen the idea of a prominent role for the endocannabinoid signalling system in the modulation of a wide variety of neurobiological functions. Among these, one of the most important is the control of movement. Cannabinoid CB1 receptors are abundantly concentrated in the basal ganglia and their activation by plant-derived or synthetic cannabinoids, as well as by their endogenous ligands, modulates the acti Read More

The opioid and cannabinoid systems share a multiplicity of effects at biochemical and behavioural levels. Both opioid and cannabinoid agonists inhibit adenylyl cyclase activity, and increase the activity of MAP kinase pathways. They also produce similar changes in the permeability of several ion channels, and inhibit neurotransmitter release. Anatomical studies show that CB1 cannabinoid receptors and mu opioid receptors ha Read More

Multiple sclerosis (MS) is a neurodegenerative disease caused by repeated inflammatory / demyelinating events within the central nervous system (CNS). In addition to relapsing-remitting neurological insults, patients are often left with residual, troublesome symptoms such as spasticity and pain. These greatly diminish “quality of life” and have prompted some patients to self-medicate and perceive benefit from cannabis. Rec Read More

The 5-HT7R is the most recent addition to the burgeoning family of serotonin receptors. Preliminary evidences suggest that it may be involved in depression, control of circadian rhythms, and relaxation in a variety of vascular smooth muscles, indicating the high potential of 5-HT7R ligands as new therapeutic drugs. During the last four years several selective 5-HT7R antagonists have been discovered, and we have recently con Read More